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CFM 1571 hydrochloride

Catalog No.GC17431

sGC activator

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CFM 1571 hydrochloride Chemical Structure

Cas No.: 1215548-30-3

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10mg
$146.00
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Sample solution is provided at 25 µL, 10mM.

Description of CFM 1571 hydrochloride

IC50: 2.84 μM for platelet

Soluble guanylate cyclase (sGC) is a key signal-transduction enzyme activated by nitric oxide (NO). Impaired bioavailability and/or responsiveness to endogenous NO has been implicated in the pathogenesis of cardiovascular and other diseases. CFM 1571 is a activator of the nitric oxide receptor, soluble guanylate cyclase.

In vitro: CFM 1571 demonstrated potent activation of soluble guanylate cyclase and potent inhibition of platelet aggregation. CFM 1571 also showed enzyme activity similar to benzydamine. CFM 1571 was additionally assayed against the NOS isoforms, and minimal inhibition was observed with iNOS (25%) and nNOS (17%). Furthermore CFM 1571 shows no significant activity at any of the other enzymes studied [1].

In vivo: Pharmacokinetic studies in rats showed that compound CFM 1571 exhibits modest oral bioavailability (12%). Furthermore 32 has an excellent selectivity profile notably showing no significant inhibition of phosphodiesterases or nitric oxide synthases [1].

Clinical trial: Up to now, CFM 1571 is still in the preclinical development stage.

Reference:
[1] Selwood DL, Brummell DG, Budworth J, Burtin GE, Campbell RO, Chana SS, Charles IG, Fernandez PA, Glen RC, Goggin MC, Hobbs AJ, Kling MR, Liu Q, Madge DJ, Meillerais S, Powell KL, Reynolds K, Spacey GD, Stables JN, Tatlock MA, Wheeler KA, Wishart G, Woo CK.  Synthesis and biological evaluation of novel pyrazoles and indazoles as activators of the nitric oxide receptor, soluble guanylate cyclase. J Med Chem. 2001 Jan 4;44(1):78-93.

Chemical Properties of CFM 1571 hydrochloride

Cas No. 1215548-30-3 SDF
Chemical Name 1-benzyl-3-(3-(dimethylamino)propoxy)-N-(4-methoxyphenyl)-1H-pyrazole-5-carboxamide hydrochloride
Canonical SMILES CN(CCCOC(C=C1C(NC2=CC=C(OC)C=C2)=O)=NN1CC3=CC=CC=C3)C.Cl
Formula C23H28N4O3.HCl M.Wt 444.95
Solubility DMSO : 100 mg/mL (224.74 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of CFM 1571 hydrochloride

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1 mg 5 mg 10 mg
1 mM 2.2474 mL 11.2372 mL 22.4744 mL
5 mM 0.4495 mL 2.2474 mL 4.4949 mL
10 mM 0.2247 mL 1.1237 mL 2.2474 mL
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In vivo Formulation Calculator (Clear solution) of CFM 1571 hydrochloride

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 27 reference(s) in Google Scholar.)

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